Mental Health Book


Benzodiazepine antagonist

Aka: Benzodiazepine antagonist, Flumazenil, Romazicon
  1. Indication
    1. Benzodiazepine sedation reversal
  2. Contraindications
    1. Mixed drug Overdose with compounds that may cause Seizure (e.g. Tricyclic Antidepressants, Cocaine)
    2. Chronic Benzodiazepine use (dependence)
    3. Seizure Disorder
  3. Dosing: Adults
    1. Benzodiazepine Sedation Reversal
      1. Initial: 0.2 mg IV over 15 seconds
      2. Titrate: 0.2 mg each minute to 1 mg total
    2. Overdose Reversal
      1. Initial: 0.2 mg IV over 30 seconds
      2. Titrate: 0.3-0.5 mg q30 seconds to 3 mg total
    3. Repeat dosing protocol
      1. Repeat Dose: 0.005 mg/kg q1-2 minutes
      2. Maximum cumulative dose: 1 mg
      3. May repeat regimen every 20 minutes
  4. Dosing: Children
    1. Initial: 0.005 to 0.2 mg IV over 3-5 minutes, titrating to effect
  5. Precautions
    1. Avoid in patients with chronic use (risks of severe withdrawal including Seizures)
      1. Most toxicology guidelines do not recommend Flumazenil in Overdose
      2. Potential harms appear to outweigh benefits in most cases
      3. Penningo (2016) Basic Clin Pharmacol Toxicol 118(1): 37-44 +PMID:26096314 [PubMed]
    2. May cause acute withdrawal if physically dependent
    3. Do not give routinely to comatose patients
      1. Only use if identity of drug is known, and certain that the patient has not used chronically
    4. Reverses Seizure protection of Benzodiazepines
      1. Increases risk of drugs that lower Seizure threshold (Cocaine, Tricyclic Antidepressants)
  6. Pharmacokinetics
    1. Onset: 1 to 2 minutes
    2. Peak: 6 to 10 minutes

Flumazenil (C0016293)

Definition (NCI) An imidazo-benzodiazepine derivative, effective in reversing benzodiazepine-induced activities. Flumazenil antagonizes the benzodiazepine binding site of the gamma-aminobutyric acid (GABA)/benzodiazepine receptor complex in the central nervous system (CNS), thereby preventing the chloride channel opening events and inhibiting neuronal hyperpolarization. As a result, flumazenil reverses benzodiazepine-induced effects including sedation, psychomotor deficits, amnesia, and hypoventilation in a dose-dependent manner.
Definition (MSH) A potent benzodiazepine receptor antagonist. Since it reverses the sedative and other actions of benzodiazepines, it has been suggested as an antidote to benzodiazepine overdoses.
Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH D005442
SnomedCT 387575000, 96247007
English Flumazenil, Flumazepil, 4H-Imidazo(1,5-a)(1,4)benzodiazepine-3-carboxylic acid, 8-fluoro-5,6-dihydro-5-methyl-6-oxo-, ethyl ester, 4H-Imidazo(1,5-a)(1,4)benzodiazepine-3-carboxylic Acid, 8-fluoro-5,6-dihydro-5-methyl-6-oxo-, Ethyl Ester, flumazenil, flumazepil, flumazenil (medication), FLUMAZENIL, Flumazenil [Chemical/Ingredient], Flumazenil (product), Flumazenil (substance)
Swedish Flumazenil
Czech flumazenil
Finnish Flumatseniili
Japanese フルマゼピル, アネキセート, フルマゼニル
Spanish flumazenil (producto), flumacenil (producto), flumacenil, flumacenil (sustancia), flumazenil (sustancia), flumazenil, Flumazenil, Flumazepil
Polish Ro 15-1788, Flumazepil, Flumazenil
French Flumazénil
German Flumazenil, Flumazepil
Italian Flumazenile
Portuguese Flumazenil, Flumazepil
Derived from the NIH UMLS (Unified Medical Language System)

Romazicon (C0591091)

Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH D005442
English Anexate, Romazicon, Hoffman La Roche Brand of Flumazenil, Hoffman-La Roche Brand of Flumazenil, Lanexat, Roche Brand of Flumazenil
Derived from the NIH UMLS (Unified Medical Language System)

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